(D) Routes of delivery: Case studies

Smith, Philip L.; Wall, Doris A.; Gochoco, Caroline H.; Wilson, Glynn

doi:10.1016/0169-409x(92)90005-b

Cited by 75 publications

(7 citation statements)

References 136 publications

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“…In general, natural occurring and unmodified peptides are usually quite hydrophilic, and its passage across the blood-brain barrier (BBB) occurs quite poorly and at very low rates [3][4][5][6]. To elicit an analgesic response in the central nervous system (CNS) after oral administration, several physico-chemical properties of opioid peptides and the passage through intractable membrane barriers via various transport systems of opioid peptides must be considered.…”

Section: Introductionmentioning

confidence: 99%

Application of liquid chromatography–tandem mass spectrometry for the determination of opioidmimetics in the brain dialysates from rats treated with opioidmimetics intraperitoneally

Igarashi

Murabayashi

Hotta

et al. 2004

Journal of Chromatography B

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Section: Introductionmentioning

confidence: 99%

Application of liquid chromatography–tandem mass spectrometry for the determination of opioidmimetics in the brain dialysates from rats treated with opioidmimetics intraperitoneally

Igarashi

Murabayashi

Hotta

et al. 2004

Journal of Chromatography B

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“…Oral administration of protein and polar macromolecular drugs usually results in extremely low to no bioavailability due to their extensive hydrolysis by acids and enzymes, and poor membrane permeability in the gastrointestinal tract (OHagan et al, 1987;Lee et al, 1991;Smith et al, 1992). In the last decade, the use of microspheres or nanoparticles to protect those drugs from degradation has been under extensive investigation (Arrieta-Molero et al, 1982;Damge et al, 1990;Morishita et al, 1992).…”

Section: Introductionmentioning

confidence: 99%

Stability Study of Drug-loaded Proteinoid Microsphere Formulations during Freeze-drying

Santiago

Chen³

et al. 1994

Journal of Drug Targeting

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Drug-loaded proteinoid microspheres were freeze-dried to facilitate shipping and handling and to enable long term storage. Heparin was chosen as the model drug in developing the optimum lyophilization process. The factors influencing the integrity of either heparin-loaded or unloaded ('empty') proteinoid microspheres during freeze-drying were determined, with emphasis on: selecting an optimum freezing and resuspending temperature; choosing an appropriate cryoprotectant and its optimum concentration in the formulation; and, designing a suitable method for formulating the microspheres. Freezing at/below -70 degrees C was found to minimize damage to the microspheres. Addition of sugars, such as trehalose and lactose, as cryoprotectants, further increased the stability of the heparin-loaded microspheres during freeze-drying. The optimum trehalose or lactose concentrations were determined to be 5% (w/v). Using the optimumized lyophilization process described in this manuscript, microspheres remained intact during freeze-drying. The freeze-dried microspheres were stable for at least three months post-lyophilization.

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“…Oral route of administration is most preferred owing to their convenience of self administration, non invasive nature and patient friendly route. As a result substantial amount of research over past decade has targeted development of alternate and/or suitable strategies to improve their oral bioavailability [78]. Oral administration of therapeutic macromolecules is notoriously difficult due to their high molecular weight, hydrophilicity, and susceptibility to enzymatic inactivation in the gastro intestinal tract (GIT).…”

Section: Oral Deilvery Of Proteinsmentioning

confidence: 99%

Novel Delivery Technologies for Protein and Peptide Therapeutics

Kumar¹,

Soppimath²,

Nachaegari³

2006

CPB

144

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The protein and peptide therapeutics have become an important class of drugs due to advancement in molecular biology and recombinant technology. There are more than 100 biopharmaceutical products approved and generating revenue of more than 56 billion US dollars. A safe, effective and patient friendly delivery of these agents is the key to commercial success. Currently, most of therapeutic proteins are administered by the parenteral route which has many drawbacks. Various delivery strategies and specialized companies have evolved over the past few years to improve delivery of proteins and peptides. Polymeric depot and PEGylation technologies have overcome some of the issues associated with parenteral delivery. A considerable research has been focused on non-invasive routes such as pulmonary, per oral and transdermal for delivery of proteins and peptides, in order to increase patient compliance yet their delivery via non-invasive routes remains challenge due to their poor absorption and enzymatic instability. Pulmonary route has shown some success evidenced by recent FDA approval of inhalable insulin. Development of an oral dosage form for protein therapeutics is still the most desirable one but with greater challenge. This review presents the issues of delivery of proteins and peptides, current and potential formulation technologies to improve delivery and current market trends.

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(D) Routes of delivery: Case studies

Cited by 75 publications

References 136 publications

Application of liquid chromatography–tandem mass spectrometry for the determination of opioidmimetics in the brain dialysates from rats treated with opioidmimetics intraperitoneally

Application of liquid chromatography–tandem mass spectrometry for the determination of opioidmimetics in the brain dialysates from rats treated with opioidmimetics intraperitoneally

Stability Study of Drug-loaded Proteinoid Microsphere Formulations during Freeze-drying

Novel Delivery Technologies for Protein and Peptide Therapeutics

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